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Y16, formerly known as RhoA-IN-Y16, is a RhoA inhibitor, Y16 blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). Y16 specifically blocks the activation of the RhoA and RhoA signaling pathways that is catalyzed by LARG. Y16 prevents the MCF7 breast cancer cells from proliferating and migrating.
| Targets |
LARG ( Kd = 76 nM )
|
|---|---|
| ln Vitro |
Y16 (10-30 μM; 24 hours; NIH 3T3 cells) is specific for RhoA and can inhibit the formation of RhoA-GTP induced by serum in a dose-dependent manner[1].
Y16 (10-30 μM; 24 hours; NIH 3T3 cells) effectively suppresses the production of phospho-MLC and phospho-FAK, which are downstream of RhoA, when induced by serum or SDF-1α[1]. |
| Cell Assay |
Cell Line: NIH 3T3 cells
Concentration: 10 μM, 30 μM Incubation Time: 24 hours Result: Inhibited RhoA-GTP formation induced by serum dose dependently and was specific for RhoA. |
| References |
| Molecular Formula |
C24H20N2O3
|
|---|---|
| Molecular Weight |
384.435
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| Exact Mass |
384.147
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| Elemental Analysis |
C, 74.98; H, 5.24; N, 7.29; O, 12.49
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| CAS # |
429653-73-6
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| Related CAS # |
429653-73-6
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| PubChem CID |
989521
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.665
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| LogP |
5.26
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
626
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1)/C(C(N1C2=CC=CC=C2)=O)=C\C3=CC(OCC4=CC(C)=CC=C4)=CC=C3
|
| InChi Key |
ITMLWGWTDWJSRZ-PXLXIMEGSA-N
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| InChi Code |
InChI=1S/C24H20N2O3/c1-17-7-5-9-19(13-17)16-29-21-12-6-8-18(14-21)15-22-23(27)25-26(24(22)28)20-10-3-2-4-11-20/h2-15H,16H2,1H3,(H,25,27)/b22-15+
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| Chemical Name |
(4E)-4-[[3-[(3-methylphenyl)methoxy]phenyl]methylidene]-1-phenylpyrazolidine-3,5-dione
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| Synonyms |
RhoA-IN-Y16; Y16; Y-16; Y 16
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~39 mg/mL (65.0~101.4 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.50 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6012 mL | 13.0059 mL | 26.0119 mL | |
| 5 mM | 0.5202 mL | 2.6012 mL | 5.2024 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6012 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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